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Dexchlorpheniramine maleate | CAS No: 2438-32-6 | GMP-certified suppliers
A medication that provides symptomatic relief for allergic rhinitis, conjunctivitis, urticaria, angioedema, and allergic reactions to transfusions by antagonizing histamine H1 receptors.
Therapeutic categories
Primary indications
- Dexchlorpheniramine can be used in the treatment of perennial and seasonal allergic rhinitis, vasomotor rhiniti, allergic conjunctivitis due to inhalant allergens and foods, mild uncomplicated allergic skin manifestations of urticaria and angioedema, amelioration of allergic reactions to blood or plasma, and dermographism
Product Snapshot
- Dexchlorpheniramine maleate is available as oral tablets, capsules, syrups, topical creams, and nasal solutions
- It is primarily used for the management of allergic conditions such as allergic rhinitis, conjunctivitis, urticaria, angioedema, and allergic reactions to blood products
- This API is approved for use in the US and Canadian pharmaceutical markets
Clinical Overview
Clinically, dexchlorpheniramine is indicated for the symptomatic treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis related to inhalant allergens and foods, mild uncomplicated allergic skin conditions including urticaria and angioedema, reactions to blood or plasma transfusions, and dermographism. Its therapeutic benefits derive from antagonism of histamine H1 receptors, providing relief from symptoms such as sneezing, watery and itchy eyes, and nasal discharge.
The pharmacodynamic profile of dexchlorpheniramine involves competitive inhibition at peripheral H1 receptors located on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. By preventing histamine binding, it mitigates hallmark features of histamine action including pruritus, vasodilation, increased vascular permeability, bronchoconstriction, and associated systemic symptoms like hypotension and tachycardia. Its mechanism of action specifically targets the histamine-mediated allergic response cascade initiated by IgE cross-linking on mast cells and basophils.
Key metabolic considerations include its role as a substrate and inhibitor of cytochrome P450 enzymes, notably CYP2D6 and CYP3A4 isoforms, indicating potential drug-drug interactions. The compound is also recognized among agents of moderate risk for QTc interval prolongation, requiring caution in susceptible populations. Additionally, it has interactions involving organic cation transporters (OCT1 and OCT2).
Safety and toxicity profiles align with central nervous system effects typical of first-generation antihistamines, such as sedation, due to blood-brain barrier penetration. Anticholinergic effects may also be present. Careful dosing and monitoring are advised in populations vulnerable to these effects.
Dexchlorpheniramine maleate is incorporated in various pharmaceutical formulations globally under multiple brand names. From a sourcing perspective, high purity and consistent stereoisomeric composition are critical attributes for API quality due to the stereoselective pharmacology. Compliance with regulatory standards and robust impurity profiling, including residual solvents and enantiomeric excess, are essential considerations in API procurement to ensure clinical efficacy and safety.
Identification & chemistry
| Generic name | Dexchlorpheniramine maleate |
|---|---|
| Molecule type | Small molecule |
| CAS | 2438-32-6 |
| UNII | B10YD955QW |
| DrugBank ID | DB09555 |
Pharmacology
| Summary | Dexchlorpheniramine is a histamine H1 receptor antagonist that competitively inhibits histamine binding on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. It reduces histamine-mediated symptoms such as vasodilation, increased vascular permeability, and bronchoconstriction associated with allergic reactions. This pharmacological action targets allergic conditions including rhinitis, conjunctivitis, urticaria, and angioedema. |
|---|---|
| Mechanism of action | Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. Dexchlorpheniramine is the predominant active isomer of chlorpheniramine and is approximately twice as active as the racemic compound. |
| Pharmacodynamics | In allergic reactions, an allergen binds to IgE antibodies on mast cells and basophils. Once this occurs IgE receptors crosslink with each other triggering a series of events that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Dexchlorpheniramine, is a histamine H1 antagonist of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
ADME / PK
| Absorption | Oral bioavailability in rats 40.5% |
|---|---|
| Half-life | 20-30 h |
| Protein binding | Dexchlorpheniramine is bound to total plasma proteins 38%, to albumin 20% and to alpha-glycoprotein acid 23%. |
| Metabolism | Hepatic metabolism. Major metabolism by CYP 2D6 and minor metabolism by 3A4, 2C11 and 2B1. |
| Route of elimination | Renal excretion |
| Volume of distribution | 321L |
| Clearance | 9.8L/h |
Formulation & handling
- Dexchlorpheniramine maleate is a small molecule primarily formulated for oral administration in various solid and liquid dosage forms, with additional topical and nasal routes available.
- Due to low water solubility and moderate lipophilicity (LogP 3.58), formulation strategies should address bioavailability challenges for oral delivery.
- Avoid concurrent use with alcohol as it may potentiate CNS depressant effects; no specific food sensitivity is noted otherwise.
Regulatory status
| Lifecycle | The API is approaching patent expiry in the US and Canada, leading to increased generic competition and market maturity in these regions. Product availability is expected to expand as exclusivity periods conclude. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Dexchlorpheniramine maleate is supplied in the US and Canadian markets through multiple branded products, indicating the presence of several originator manufacturers. The product's availability under various brand names suggests established global marketing, primarily focused on North America. The absence of specific patent information limits assessment of generic competition, but multiple brands imply existing generic or non-originator presence. |
|---|
Safety
| Toxicity | Central nervous system depression |
|---|
- May cause central nervous system depression
- Handle with appropriate ventilation and avoid inhalation of dust or vapors
- Use personal protective equipment to prevent dermal and ocular exposure
Dexchlorpheniramine maleate is a type of Antihistamines
Antihistamines are a vital subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the treatment of allergies and allergic reactions. These compounds work by blocking the action of histamines, which are responsible for triggering allergic symptoms such as itching, sneezing, runny nose, and watery eyes.
Antihistamines can be classified into two main categories: first-generation and second-generation antihistamines. First-generation antihistamines, such as diphenhydramine and chlorpheniramine, have been in use for several decades. They are effective in relieving allergy symptoms but are associated with drowsiness and other side effects due to their ability to cross the blood-brain barrier.
On the other hand, second-generation antihistamines, including cetirizine, loratadine, and fexofenadine, offer similar allergy relief with fewer sedative effects. These newer antihistamines are preferred for their improved safety profiles, making them suitable for use during the day without causing significant drowsiness.
Antihistamines are available in various forms, including tablets, capsules, syrups, and topical creams. They are extensively used to manage conditions such as hay fever, hives, allergic rhinitis, and insect bites. Moreover, antihistamines may also be combined with decongestants or other medications to provide relief from nasal congestion and sinus symptoms.
As pharmaceutical APIs, antihistamines are produced through meticulous synthesis and manufacturing processes, adhering to strict quality standards. These APIs serve as the active components in various branded and generic pharmaceutical formulations, making them crucial in the pharmaceutical industry's production of allergy medications.
In conclusion, antihistamines are a significant subcategory of pharmaceutical APIs widely used for alleviating allergy symptoms. Their classification into first- and second-generation antihistamines offers options based on efficacy and sedative effects. By blocking histamines, antihistamines provide relief from common allergic reactions, making them essential in the development of effective allergy medications.
Dexchlorpheniramine maleate (Antihistamines), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Dexchlorpheniramine maleate API manufacturers & distributors
Compare qualified Dexchlorpheniramine maleate API suppliers worldwide. We currently have 6 companies offering Dexchlorpheniramine maleate API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Keshava Organics | Producer | India | India | CoA, USDMF, WC | 6 products |
| Kongo Chemical | Producer | Japan | Japan | CEP, CoA, FDA, USDMF | 5 products |
| Pharm Rx Chemical Corp | Distributor | United States | India | BSE/TSE, CoA, GMP, MSDS, USDMF | 166 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Tresinde Biotech | Producer | India | India | CoA, GMP | 50 products |
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